Journal: bioRxiv

Article Title: Pathway Coessentiality Mapping Reveals Complex II is Required for de novo Purine Biosynthesis in Acute Myeloid Leukemia

doi: 10.1101/2025.02.26.640463

Figure Lengend Snippet: a-c) Effect of Complex II inhibition by TTFA on levels of de novo purines (a) IMP, (b) AMP/dGMP, and (c) GMP. AMP/dGMP cannot be resolved based on mass spectrometry separation. d) Effect of exogenous purines (adenine (A), guanine (G), hypoxanthine (H), inosine (I)) or pyrimidines (cytidine (C), uridine (U), thymidine (T)) on viability in MOLM-13 cells treated with the targeted purine synthesis (GART) inhibitor, lometrexol (LTX). Each nucleotide species was added back at a concentration of 30 μM. e) Effect of exogenous purines or pyrimidines on viability in MOLM-13 cells treated with dihydroorotate dehydrogenase (DHODH) inhibitor, brequinar (2 μM). f-h) Data were analyzed using one-way ANOVA with a Tukey post-hoc test.

Article Snippet: Brequinar was purchased from MedChem Express.

Techniques: Inhibition, Mass Spectrometry, Concentration Assay

Journal: Cell reports

Article Title: EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer

doi: 10.1016/j.celrep.2022.111827

Figure Lengend Snippet:

Article Snippet: Brequinar , Selleckchem , Cat#S6626; CAS: 96187-53-0.

Techniques: Microarray, Recombinant, Purification, Membrane, SYBR Green Assay, Viability Assay, Phospho-proteomics, Kinase Assay, Reverse Transcription, Transcription Factor Assay, Enzyme-linked Immunosorbent Assay, Multiplex Assay, Extraction, Isolation, shRNA, Sequencing, Plasmid Preparation, Software

Journal: Cell metabolism

Article Title: Induction of a Timed Metabolic Collapse to Overcome Cancer Chemoresistance

doi: 10.1016/j.cmet.2020.07.009

Figure Lengend Snippet: KEY RESOURCES TABLE

Article Snippet: Brequinar (BRQ) , Broad Institute , N/A.

Techniques: Recombinant, Labeling, RNA Sequencing, shRNA, Software

Journal: Data in Brief

Article Title: Screening of potential antiviral molecules against equid herpesvirus-1 using cellular impedance measurement: Dataset of 2,891 compounds.

doi: 10.1016/j.dib.2020.106492

Figure Lengend Snippet: Screening of 41 compounds (in-house antiviral library) selected for their effects against different human viruses at 4 concentrations (0.4, 2, 10 and 50 µM). For each compound, the following values are provided: the area under normalised Cell Index curve (AUC n ), the %AUC n compared to AUC n of untreated infected cells, the time required for the cell index to decrease by 50 % after virus infection (CIT 50 ) and the ΔCIT 50 value obtained by comparing results for treated vs untreated, EHV-1-infected control wells. The Z’-factor was used to assess the quality of the screening in 96-well format. For untreated mock-infected and untreated infected cells, the mean ± SD of AUC n is reported. N.D., not determinable.

Article Snippet: Brequinar , Adooq Bioscience , 0.78 , 8.93 , 19.30 , 33.42 , 30.61 , −55.11 , −27.84 , 9.33 , 1.94 , 0:22:31 , 25:28:27 , 36:12:01 , 33:25:59 , −29.84 , −4.74 , 5.99 , 3.22.

Techniques: Infection, Virus, Control

Journal: RSC Medicinal Chemistry

Article Title: Radiosynthesis of [ 18 F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers †

doi: 10.1039/d4md00433g

Figure Lengend Snippet: Cu-catalyst that influence the RCC of [ 18 F]brequinar

Article Snippet: Brequinar is one of the most potent hDHODH inhibitors so far discovered (IC50 1.8 nM in recombinant hDHODH).25,26 Originally developed by DuPont (DuP-785) in 1985,27 it was acquired from Bristol Myers Squibb by Clear Creek Bio, which has recently supported phase I/II clinical trials for the treatment of patients with relapsed/refractory AML (NCT03760666).28.

Techniques: Radioactivity, Solvent

Journal: RSC Medicinal Chemistry

Article Title: Radiosynthesis of [ 18 F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers †

doi: 10.1039/d4md00433g

Figure Lengend Snippet: Protected [ 18 F]brequinar (intermediate) recovery (%) on using various cartridges eluted with acetonitrile

Article Snippet: Brequinar is one of the most potent hDHODH inhibitors so far discovered (IC50 1.8 nM in recombinant hDHODH).25,26 Originally developed by DuPont (DuP-785) in 1985,27 it was acquired from Bristol Myers Squibb by Clear Creek Bio, which has recently supported phase I/II clinical trials for the treatment of patients with relapsed/refractory AML (NCT03760666).28.

Techniques:

Journal: RSC Medicinal Chemistry

Article Title: Radiosynthesis of [ 18 F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers †

doi: 10.1039/d4md00433g

Figure Lengend Snippet: [ 18 F]Brequinar hydrolysis reaction conditions (reagent, equivalents, temperature, and time)

Article Snippet: Brequinar is one of the most potent hDHODH inhibitors so far discovered (IC50 1.8 nM in recombinant hDHODH).25,26 Originally developed by DuPont (DuP-785) in 1985,27 it was acquired from Bristol Myers Squibb by Clear Creek Bio, which has recently supported phase I/II clinical trials for the treatment of patients with relapsed/refractory AML (NCT03760666).28.

Techniques: Solvent

Journal: RSC Medicinal Chemistry

Article Title: Radiosynthesis of [ 18 F]brequinar for in vivo PET imaging of hDHODH for potential studies of acute myeloid leukemia and cancers †

doi: 10.1039/d4md00433g

Figure Lengend Snippet: pH influence on HPLC purification of [ 18 F]brequinar

Article Snippet: Brequinar is one of the most potent hDHODH inhibitors so far discovered (IC50 1.8 nM in recombinant hDHODH).25,26 Originally developed by DuPont (DuP-785) in 1985,27 it was acquired from Bristol Myers Squibb by Clear Creek Bio, which has recently supported phase I/II clinical trials for the treatment of patients with relapsed/refractory AML (NCT03760666).28.

Techniques: Purification, Solvent

Journal:

Article Title: New Immunosuppressive Drugs: Mechanistic Insights and Potential Therapeutic Advances

doi:

Figure Lengend Snippet: Diversity and modes of action of “new” immunosuppressive drugs

Article Snippet: Brequinar sodium (quinoline carboxylic acid derivative) , Dupont-Merck Pharmaceutical Co., Wilmington, DE , No , Makowka & Cramer 1992 , 1993.

Techniques: DNA Synthesis, Activation Assay

Journal:

Article Title: New Immunosuppressive Drugs: Mechanistic Insights and Potential Therapeutic Advances

doi:

Figure Lengend Snippet: Structure of brequinar sodium (BQR) superimposed on a flow diagram to indicate the probable sites of action of the drug on pyrimidine biosynthesis. Sites of enzyme action are denoted by numbers in parentheses. In addition to inhibiting dihydroorotate dehydrogenase, our recent observations indicate that BQR also inhibits cytidine deaminase. The enzymes involved in the pathway are (1) dihydroorotate dehydrogenase; (2) orotate phosphoribosyltransferase, orotidine 5′– monophosphate decarboxylase, nucleoside monophosphate kinase and nucleoside disphosphate kinase (in sequence along the pathway); (3) nucleoside kinase; (4) cytidine deaminase and (5) CTP synthetase. CTP=cytidine triphosphate; UTP = uridine triphosphate.

Article Snippet: Brequinar sodium (quinoline carboxylic acid derivative) , Dupont-Merck Pharmaceutical Co., Wilmington, DE , No , Makowka & Cramer 1992 , 1993.

Techniques: Sequencing